2017
DOI: 10.1007/s00726-017-2526-y
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Pre-clinical study of a TNFR1-targeted 18F probe for PET imaging of breast cancer

Abstract: Tumor necrosis factor receptor 1 (TNFR1) is overexpressed in several varieties of carcinoma, including breast cancer. WH701 (Ala-Thr-Ala-Gln-Ser-Ala-Tyr-Gly), which was identified by phage display, can specifically bind to TNFR1. In this study, we labeled WH701 with F and investigated its tumor diagnostic value. WH701 was synthesized by standard Fmoc-solid phase synthetic protocols and conjugated by NOTA-NHS. NOTA-WH701 was radiolabeled withF using NOTA-AlF chelation reaction. The tumor target properties were … Show more

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Cited by 10 publications
(5 citation statements)
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“…In clinical development, there are only a few d -peptides and l -RNA aptamers that can target naturally existing l -small proteins or -peptide epitopes, , most likely because preparation of d -protein targets is rather difficult. A simple route to d -TNFR-1 CRD2 may facilitate the discovery of ultrastable, chirally inverted molecules targeting TNFR-1, which can be potentially applied in the studies related to inflammatory diseases. ,,, For example, d -peptide ligands targeting the TNFR-1 may be coupled with a chemical reporter, such as florescent- or radiolabeling, and utilized for the imaging/detection of TNFR-1 distributions . The TNFR-1 CRD2 synthesis scheme may also find uses in other biophysical and -physiological studies such as the investigation of specific post-translational modifications or the development of novel TNF-α biosensors .…”
Section: Discussionmentioning
confidence: 99%
“…In clinical development, there are only a few d -peptides and l -RNA aptamers that can target naturally existing l -small proteins or -peptide epitopes, , most likely because preparation of d -protein targets is rather difficult. A simple route to d -TNFR-1 CRD2 may facilitate the discovery of ultrastable, chirally inverted molecules targeting TNFR-1, which can be potentially applied in the studies related to inflammatory diseases. ,,, For example, d -peptide ligands targeting the TNFR-1 may be coupled with a chemical reporter, such as florescent- or radiolabeling, and utilized for the imaging/detection of TNFR-1 distributions . The TNFR-1 CRD2 synthesis scheme may also find uses in other biophysical and -physiological studies such as the investigation of specific post-translational modifications or the development of novel TNF-α biosensors .…”
Section: Discussionmentioning
confidence: 99%
“…Thus, these molecules may be considered to be potential therapeutic targets. To date, the commercial antibodies, antagonists, and small-molecule inhibitors against TNF, TNFR, TNFR1, and TNFR2 have been successfully used to treat several human autoimmune diseases, such as rheumatoid arthritis, inflammatory bowel disease, and psoriasis [56][57][58][59][60]. Taken together, to increase the efficacy of anti-tumor treatment with anti-TNFR-related reagents, it may be important to examine the alterations in TNFR1, TNFR2, and TNF levels and Treg cell numbers in human lung tumors.…”
Section: Conclusion and Therapeutic Perspectivementioning
confidence: 99%
“…WH701 was screened from the phage 6-mer peptide library, which is a kind of random library. DAvp-1 and WH701 can both specifically bind to TNFR1 [ 76 , 77 ].…”
Section: The Peptides Obtained According To Different Targets Related...mentioning
confidence: 99%